RT Journal Article
SR Electronic
T1 Development of Narrow Spectrum ATP-competitive Kinase Inhibitors as Probes for BIKE and AAK1
JF bioRxiv
FD Cold Spring Harbor Laboratory
SP 094631
DO 10.1101/094631
A1 Rafael M. Couñago
A1 Alison D. Axtman
A1 Hátylas Azevedo
A1 David H. Drewry
A1 Jonathan M. Elkins
A1 Opher Gileadi
A1 Cristiano R. W. Guimarães
A1 Alessandra Mascarello
A1 Carrow I. Wells
A1 Timothy M. Willson
A1 William J. Zuercher
YR 2016
UL http://biorxiv.org/content/early/2016/12/15/094631.abstract
AB Understanding the structural determinants of inhibitor selectivity would facilitate the design and preparation of kinase probes. We describe a pair of matched compounds differing only by one degree of saturation but showing dramatic differential activities at select kinases. We utilized x-ray crystallography and computational analysis to rationalize the basis of the differential activity.